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. 2020 May 6;7:75. doi: 10.3389/fmolb.2020.00075

TABLE 2.

Summary of testing of ADAM10 selective inhibitors with various cell-based ADAM10 and synthetic substrates.

Target Cell line Glycosylation type Position [C] tested, μM CID3117694, %inhibition (IC50, μM) GI254023X, %inhibition
TNFα non-glycosylateda N/A None N/A 0.01–100 18 (>100) 100
TNFα glycosylateda N/A Gal-GalNAc S4 0.01–100 100 (1.1) 100
HER2a BT474 GlcNAc Multiple (Yuan et al., 2003) 10 0 100
CXCL16a A549 Gal-GalNAc Multiple (Abel et al., 2004) 10 80 100
Syndecan-4a A549 Heparan Sulfate S39, S61, S63 (Bernfield et al., 1992) 10 0 100

NT, not tested. aMadoux et al. (2016).